Tertiapin-Q

CAT#

R1101

CAS No.

910044-56-3

Description

Tertiapin Q is a stable derivative of the bee venom toxin tertiapin. It is a high affinity blocker for inward-rectifier K+ channels that binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with high affinity (Ki values are 1.3 and 13.3 nM respectively).

Background

Tertiapin-Q (TPNQ) is a derivative of honey bee toxin tertiapin (TPN) whose methionine residue is replaced with a glutamine residue. TPNQ inhibits the ROMK1 and GIRK1/4 inward-rectifier K+channels with affinities very similar to TPN. However, unlike native TPN, TPNQ is nonoxidizable by air. >> Read More

References

The stability of TPNQ allows us to investigate how it interacts with the targeted channels. We found that the interaction between TPNQ and the ROMK1 channel is a bimolecular reaction, i.e., one TPNQ molecule binds to one channel. The interaction surface in TPNQ is primarily formed by its α helix rather than the β sheets with which scorpion toxins form their interaction surface. The mutagenesis studies on both the channel and TPNQ together strongly suggest that to block the K+pore TPNQ plugs its α helix into the vestibule of the K+ pore, while leaving the extended structural portion sticking out of the vestibule into the extracellular media.

Mechanisms of Inward-Rectifier K+ Channel Inhibition by Tertiapin-Q

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